Landon R. Whitby

TL;DR: This work uses activity-based protein profiling coupled with quantitative mass spectrometry to globally map the targets, both specific and non-specific, of covalent kinase inhibitors in human cells and shows that, when these windows are exceeded, rampant proteome-wide reactivity and kinase target-independent cell death conjointly occur.

TL;DR: The discovery of a small molecule inhibitor of the kinase reaction of PKR is reported, which was discovered by screening a library of 26 different ATP-binding site directed inhibitors of varying structure.

TL;DR: The design and solution-phase synthesis of an alpha-helix mimetic library as an integral component of a small-molecule library targeting protein-protein interactions are described and suggest that a digestion of the initial screening results that accompany the use of such a comprehensive library can provide insights into the nature of the interaction.

TL;DR: Neoseptins are described, chemically synthesized peptidomimetics that bear no structural similarity to the established TLR4 ligand, lipopolysaccharide (LPS), but productively engage the mouse TLR 4 (mTLR4)/myeloid differentiation factor 2 (MD-2) complex.

TL;DR: The results suggest that the use of such comprehensive libraries of peptide secondary structure mimetics, built around effective molecular scaffolds, constitutes a powerful method of interrogating PPIs.